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Compound low-molecular heparin sodium liposome gel and preparation method and application thereof

A technology of low-molecular-weight heparin sodium and body gel, which is applied in the field of medicine and can solve the problems of high molecular weight, poor water-solubility and fat-solubility, and difficult transdermal absorption.

Inactive Publication Date: 2013-10-23
SHENZHEN HEPALINK PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, low-molecular-weight heparin sodium is a polyanionic hydrophilic compound with a large molecular weight (average molecular weight of 3000-8000 Da), and it is difficult to penetrate the stratum corneum of the skin.
And asiaticoside is a weakly acidic compound that is difficult to ionize, with a large molecular weight (C 48 h 78 o 19 ,M r :959.15Da), water-soluble and fat-soluble are poor, difficult to transdermal absorption

Method used

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  • Compound low-molecular heparin sodium liposome gel and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Take madecassoside 1.0g, egg yolk lecithin 2.0g, cholesterol 500mg, octadecylamine 40mg, add 5mL ethanol, dissolve completely and form lipid solution; dissolve 14000IU low molecular weight heparin sodium, 200mg sodium cholate in phosphoric acid In the salt buffer solution; the lipid solution is slowly injected into the above-mentioned phosphate buffer solution under stirring to make a liposome coarse dispersion solution with a weight of 20 g; the liposome coarse dispersion solution is ultrasonically treated (300W, 5min, on5s , off5s) to obtain compound low molecular weight heparin sodium liposome suspension.

[0026] Take 0.4g of Carbomer 940, add 4.0g of 1,2-propanediol to wet and disperse; take 0.12g of allantoin and dissolve it in phosphate buffer solution, add it to the 1,2-propanediol dispersed with Carbomer 940, After mixing and swelling overnight, adjust the pH to 6.5 with triethanolamine, and stir evenly to form a blank gel with a weight of 20 g.

[0027]The co...

Embodiment 2

[0029] Take 0.5g of asiaticoside, 1000mg of soybean lecithin, 150mg of cholesterol, 40mg of cetyltrimethylammonium bromide, add 4mL of ethanol, completely dissolve to form a lipid solution; mix 8000IU low molecular weight heparin sodium, 100mg Sodium deoxycholate is dissolved in purified water; the lipid solution is slowly injected into the above-mentioned solution under stirring to make a coarse liposome dispersion solution with a weight of 20 g; the coarse dispersion solution of liposome is processed by a high-pressure homogenizer (800bar, 3cycles) to obtain compound low molecular weight heparin sodium liposome suspension.

[0030] Take 0.4g of menthol, add 4.0g of 1,2-propanediol to dissolve it, add 3.2g of hypromellose, stir to disperse it; take 0.1g of allantoin and dissolve it in purified water, and dissolve it with 1mol / L hydrochloric acid Adjust the pH to 6.5; add 1,2-propanediol dispersed with hypromellose and menthol into the pH 6.5 solution dissolved with allantoin,...

Embodiment 3

[0033] Take 100mg of asiaticoside, 500mg of egg yolk lecithin, 100mg of cholesterol, 20mg of stearylamine, add 3mL of ethanol, and form a lipid solution after completely dissolving; dissolve 4000IU of low molecular weight heparin sodium and 100mg of Tween 80 in water for injection The lipid solution was slowly injected into the water for injection under stirring to make a coarse liposome dispersion solution with a weight of 20 g; the liposome coarse dispersion solution was subjected to ultrasonic treatment (600W, 3min, on5s, off5s) to obtain compound low molecular weight heparin Sodium liposomal suspension.

[0034] Take 0.8g of sodium carboxymethyl cellulose, add 4.0g of 1,2-propylene glycol, wet and disperse; take 0.04g of allantoin and dissolve it in water for injection, adjust the pH to 6.5 with 1mol / L hydrochloric acid, and add it to In 1,2-propylene glycol dispersed with sodium carboxymethylcellulose, stir evenly to form a blank gel with a weight of 20 g.

[0035] The c...

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Abstract

The invention belongs to the technical field of medicines and relates to a compound low-molecular heparin sodium liposome gel and a preparation method and application thereof. The compound low-molecular heparin sodium liposome gel comprises low-molecular heparin sodium, asiaticoside, lipid components, a membrane softening agent and gel matrix components, wherein the low-molecular heparin sodium and asiaticoside are pharmacological active ingredients, and based on the total gel of 100g, the content of the low-molecular heparin sodium is 5000-35000IU, and the content of the asiaticoside is 0.1-2.5g. The preparation method comprises the following steps of: (1) preparing a compound low-molecular heparin sodium liposome by employing an ethanol injection-ultrasonic method or ethanol injection-high pressure homogenizer method; (2) preparing a blank gel; (3) adding the compound low-molecular heparin sodium liposome into the blank gel, uniformly stirring, and obtaining the compound low-molecular heparin sodium liposome gel. The gel is mainly used for treating skin injury and scar.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a liposome gel of compound low-molecular-weight heparin sodium and asiaticoside and a preparation method thereof. The gel is mainly used for treating skin damage and scars. Background technique [0002] Scar refers to physical, chemical, biological and other damaging factors acting on human skin tissue, resulting in severe damage that cannot be repaired normally, and replaced by fibrous tissue, leaving local symptoms that affect both appearance and function. The main causes of scars are trauma, surgery, burns, acne and so on. Scars sometimes bring great mental and physical pain to patients. The current scar treatment methods mainly include surgery, physical therapy and drug therapy. Surgical treatment, such as surgical resection, grinding, etc., these treatments are invasive treatments, which may lead to secondary scars; physical therapy, such as mechanical compression, freezing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/727A61K9/127A61K9/06A61K47/18A61K47/28A61K47/34A61P17/02A61K31/7024
Inventor 刘敏敏马小来李锂
Owner SHENZHEN HEPALINK PHARMA GRP CO LTD
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